ARTESUNATE
Astemizole is a longacting antihistamine that blocks peripheral H1 receptors. Withdrawn in many regions due to QT prolongation risks. Side effects include arrhythmias and dizziness. Only GMP materials will be supplied, logistics all according to GDP.
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Product Description
Mechanism of action
Artesunate is a semi-synthetic derivative of artemisinin in which a hemisuccinate group enhances water solubility. It is rapidly hydrolysed in vivo to dihydroartemisinin, the primary active metabolite. Dihydroartemisinin exerts potent antimalarial activity by interacting with intraparasitic ferrous iron or haem to generate reactive oxygen species and carbon-centred radicals. These radicals alkylate vital parasitic proteins and membrane components, disrupting mitochondrial and endoplasmic reticulum function and leading to rapid parasite death, particularly in the ring and early trophozoite stages of Plasmodium species.
Benefits and advantages
Artesunate is a key component of artemisinin-based combination therapies (ACTs) for severe and uncomplicated malaria. In research it is indispensable for studying fast-acting schizonticidal mechanisms, parasite clearance dynamics, resistance mutations in K13 and related loci, and pharmacokineticpharmacodynamic modelling of ACT regimens. Its high aqueous solubility allows intravenous and intramuscular formulations for severe malaria models.
Side effects and risks
Potential risks include transient neutropenia, haemolysis (especially delayed haemolytic anaemia in some patients), hepatic enzyme elevations and hypersensitivity reactions. In concentrated form, it should be handled as a potent bioactive compound with appropriate containment and protection from light and moisture.
Only GMP materials will be supplied, logistics all according to GDP.
Datasheet
| Molecular Formula | C19H28O8 |
|---|---|
| Molecular Weight | 384.4 g/mol |
| CAS Number | 88495-63-0 |
| Storage Condition | Store in a cool, dry place. Keep container tightly closed. Protect from moisture and light. |
| Solubility | Solubility depends on solvent and conditions (e.g., pH). Please contact us for solvent-specific guidance. |
| Purity | Purity information is available upon request (COA). |
| Synonym | Artesunate; Artesunic acid; 88495-63-0; Arsumax; Plasmotrin |
| IUPAC/Chemical Name | 4-oxo-4-[[(1R,4S,5R,8S,9R,10S,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-yl]oxy]butanoic acid |
| InChl Key | FIHJKUPKCHIPAT-AHIGJZGOSA-N |
| InChl Code | InChI=1S/C19H28O8/c1-10-4-5-13-11(2)16(23-15(22)7-6-14(20)21)24-17-19(13)12(10)8-9-18(3,25-17)26-27-19/h10-13,16-17H,4-9H2,1-3H3,(H,20,21)/t10-,11-,12+,13+,16-,17-,18-,19-/m1/s1 |
| References |
3D Conformer.
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